MK-571

MK-571 is a cysteinyl leukotriene 1 (CysLT1) receptor antagonist (Ki = 2.1 nM in a radioligand binding assay using isolated human lung membranes). It inhibits contractions induced by leukotriene D4 (LTD4, Cay-20310) or LTE4 (Cay-20410) in histamine-primed isolated guinea pig trachea (pA2s = 9.4 and 9.1, respectively), but does not inhibit contractions induced by LTC4 (Cay-20210) in histamine-primed isolated guinea pig trachea when used at a concentration of 190 nM. MK-571 (100 nM) inhibits LTD4-induced calcium mobilization in COS-7 monkey kidney cells expressing the human CysLT1 receptor in a reporter assay. MK-571 (5 mg/kg) improves tissue damping and elasticity, markers of lung function, and decreases IL-4 and IL-5 levels in bronchoalveolar lavage fluid (BALF) in a mouse model of ovalbumin-induced asthma.Formal Name: 3-[[[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl][[3-(dimethylamino)-3-oxopropyl]thio]methyl]thio]-propanoic acid. CAS Number: 115104-28-4. Synonyms: L-660,711. Molecular Formula: C26H27ClN2O3S2. Formula Weight: 515.1. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, Ethanol: 1 mg/ml. lambdamax: 226, 283, 327, 344, 357 nm. SMILES: ClC1=CC=C2C(N=C(/C=C/C3=CC=CC(C(SCCC(O)=O)SCCC(N(C)C)=O)=C3)C=C2)=C1. InChi Code: InChI=1S/C26H27ClN2O3S2/c1-29(2)24(30)12-14-33-26(34-15-13-25(31)32)20-5-3-4-18(16-20)6-10-22-11-8-19-7-9-21(27)17-23(19)28-22/h3-11,16-17,26H,12-15H2,1-2H3,(H,31,32)/b10-6+. InChi Key: AXUZQJFHDNNPFG-UXBLZVDNSA-N.